Udenafil

Catalog No.S6433

For research use only.

Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.

Udenafil Chemical Structure

CAS No. 268203-93-6

Purity & Quality Control

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Biological Activity

Description Udenafil is a potent antagonist of human PDE5 with an IC50 of 8.25 nM and a comparable selectivity profile as sildenafil for the other PDEs.
Targets
PDE5 [1]
(Cell-free assay)
PDE3 [1]
(Cell-free assay)
PDE6 [1]
(Cell-free assay)
PDE2 [1]
(Cell-free assay)
8.25 nM 52 nM 53.3 nM 101 nM
In vitro

The inhibitory effect of udenafil on PDE5 is about 150-fold greater than that on PDE1 (selectivity ratio of 149). PDE11 selectivity of udenafil (selectivity ratio of 96) is relatively high, indicating a very low probability of inhibition of PDE11 at therapeutic doses of udenafil. The IC50 values for PDE2, PDE3, and PDE6 of udenafil are 101±15.1 nM, 52.0±3.53 nM, and 53.3±2.47 nM respectively[1].

In vivo

Udenafil is rapidly absorbed, reaching peak plasma concentrations at 0.8-1.3 h, then declining monoexponentially with a terminal half-life (T1/2) between 7.3 and 12.1 hours, giving it the unique pharmacokinetics of both relatively rapid onset and long duration. Udenafil has also been shown in preclinical studies to have potent erectogenic properties in rats and rabbits with a broad safety margin[2]. Absolute oral bioavailability of udenafil is only 38% in rats. This low oral bioavailability of udenafil appears to be mainly due to a considerable intestinal first-pass effect[1].

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(193.55 mM)
Ethanol 25 mg/mL
(48.38 mM)
Water Insoluble

Chemical Information

Molecular Weight 516.66
Formula

C25H36N6O4S

CAS No. 268203-93-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NN(C2=C1N=C(NC2=O)C3=C(C=CC(=C3)S(=O)(=O)NCCC4CCCN4C)OCCC)C

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01928563 Unknown status Drug: Dapoxetine|Drug: Udenafil|Drug: Udenafil+Dapoxetine Healthy Male Subjects Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. September 2013 Phase 1
NCT01929213 Unknown status Drug: Udenafil|Drug: Bosentan|Drug: Udenafil/Bosentan Healthy Volunteers Dong-A Pharmaceutical Co. Ltd.|Dong-A ST Co. Ltd. August 2013 Phase 1
NCT01108900 Completed Drug: sildenafil Erectile Dysfunction Pfizer''s Upjohn has merged with Mylan to form Viatris Inc.|Pfizer July 2010 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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